Time-Dependent Inactivation of Human Placental Aromatase by Bromoacetoxy 4-Androsten-3-ones in the Presence of Reduced Nicotinamide Adenine Dinucleotide Phosphate (NADPH)

スポンサーリンク

概要

• 論文の詳細を見る

• 6-Bromoacetoxyandrostenediones (1 and 2) and 17β-bromoacetoxy-4-androsten-3-one having a 6β-bromo (3), 6-keto (4), 6β-methoxyl (5) substituent were evaluated as mechanism-based inactivators of human placental aromatase. All of these compounds except the 6α-bromoacetate 1 showed a time-dependent, pseudo-first-order inactivation of aromatase in the presence of reduced nicotinamide adenine dinucleotide phosphate (NADPH) with apparent K_i's of 40,50,30,and 34 μM and k_<inact>'s of 0.048,0.364,0.267,and 0.040 min^<-1>, respectively, for compounds 2,3,4,and 5. The enzyme inactivation with compounds 3 and 4 was blocked by the addition of the substrate androstenedione to the incubates, and NADPH and oxygen were required for their effective time-dependent inactivation.

• 公益社団法人日本薬学会の論文
• 1989-03-25

著者

• 沼沢 光輝

  Tohoku Pharmaceutical University

• 沼沢 光輝

  Tohoku College Of Pharmacy

• Nagaoka M

  Tohoku Pharmaceutical Univ. Sendai Jpn

• Nagaoka Masao

  Tohoku College Of Pharmacy:sankyo Co. Ltd.

• 睦見 綾子

  Tohoku College of Pharmacy

• 長岡 正男

  Tohoku College of Pharmacy

• 辻 正親

  Tohoku College of Pharmacy

関連論文

• アロマターゼの自殺基質ATとシステインとの反応性
• Conformational Analysis of 19-Oxygenated Steroids with a 4-Ene or 2,4-Diene Structure, Potential Intermediates of Aromatase Reaction, with Semiempirical Molecular Orbital PM3 Calculations
• C(10)-C(19) Bond Cleavage Reaction of 19-Oxygenated Androst-4-ene-3,6-dione Steroids under Various Conditions
• Improved Synthesis and Molecular Modeling of 4β,19-Dihydroxyandrost-5-en-17-one, an Excellent Inhibitor of Aromatase
• Androst-4-ene-17-thione とその 5-ene 異性体の合成とアロマターゼ阻害活性
• Aromatization of 19-Oxygenated Androst-4-ene-3,6,17-triones with Human Placental Microsomes
• Biochemical Studies of Estr-4-ene-3,6,17-trione and 5α-Androstan-17-ones with or without a Carbonyl Function at C-3 and/or C-6 as Aromatase Inhibitors
• キャピラリーFTD-GCによる玄米および大豆中15種有機含窒素系農薬の一斉分析法
• アロマターゼ自殺基質Androst-4-ene-3,6,17-trioneの19位酸素化体とN-Acetyl-_L-cysteineとの1,4-付加反応
• Synthesis of Deuterium-Labeled 16α, 19-Dihydroxy C_ Steroids as Internal Standards for Gas Chromatography-Mass Spectrometry
• A Radiometric Assay Method for Aromatase Activity Using [1β-^3H]16α-Hydroxyandrostenedione
• Competitive Inhibition and Suicide Inactivation of Human Placental Aromatase by Androst-4-ene-3,6-dione Derivatives and 3α-Methoxyandrost-4-ene-6,17-dione
• Synthesis of 16α-Hydroxyandrost-4-ene-3,17,19-trione and 3β, 16α-Dihydroxyandrost-5-ene-17,19-dione : Potential Intermediates of Estriol Biosynthesis
• Oxygenation of 2,4-Dibromoestrogens with Nitric Acid : A New Synthesis of 19-Nor Steroids
• Radioimmunoassay of 2-Hydroxyestrone Using Antisera Raised against Antigenic Complexs Obtained by Convenient Methods
• Time-Dependent Inactivation of Human Placental Aromatase by Bromoacetoxy 4-Androsten-3-ones in the Presence of Reduced Nicotinamide Adenine Dinucleotide Phosphate (NADPH)
• Reactions of Enolizable Steroidal 4-En-3-ones and 17-Ones with Hypervalent Iodine
• Stereospecific 1,2-Hydride Shift in the Rearrangement of 16β-Hydroxy-17-oxo Steroids to 17β-Hydroxy-16-ones with Acid and Base(Organic,Chemical)
• Preparation of [1,2-^3H,4-^C]16α-Hydroxyandrostenedione and Its Use for Radiometric Determination of Human Placental Aromatase Activity(Analytical,Chemical)
• Regiospecific Deoxygenation of the Dihydroxyacetone Moiety at C-17 of Corticoid Steroids with Iodotrimethylsilane
• Reaction of 21-Bromo-17α-methoxy-20-ketopregnenes with Sodium Methoxide or Potassium Acetate
• Synthesis of Deuterium-Labelled 16α-Hydroxy-4-androstene-3,17-dione and 16α-Hydroxydehydroepiandrosterone
• Synthesis of Deuterium-labelled Estriol, 16α-Hydroxyestrone and Estriol 16-Glucuronide via 2,4,16α-Tribromoestrone as Internal Standards for Mass Fragmentography
• 急性心筋梗塞のマ-カ-酵素としてのクレアチンキナ-ゼ
• Purification and Characterization of Sialidase from Porcine Liver
• Effects of Inorganic Anions on the Activation of Acid Sialidases
• Effect of Sulfated Compounds on Acid Sialidase
• Identification of 16α, 19-Dihydroxyandrostenedione in the Serum of Pregnant Women by Gas Chromatography-Mass Spectrometry
• DETERMINATION OF AROMATASE ACTIVITY INVOLVED IN THE FORMATION OF ESTRIOL WITH HUMAN PLACENTAL MICROSOMES AND ITS KINETIC PROPERTIES
• Formation of 17β-Alkoxy-16-keto Steroids by Reaction of 16α-Hydroxy-17-keto and 17β-Hydroxy-16-keto Steroids with Trimethylsilyl Iodide in the Presence of Alkyl Alcohols
• Mechanistic Studies of Deoxygenation of Steroidal Ring-D 16,17-Ketols with trimethylsilyl Iodide
• Deoxygenation of Steroidal Ring-D 16,17-Ketols with Trimethylsilyl Iodide

もっと見る 閉じる

スポンサーリンク